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Inhibition of Btk by Btk-specific concentrations of ibrutinib and acalabrutinib delays but does not block platelet aggregation to GPVI

Nicolson, P. L. R.; Hughes, C. E.; Watson, S.; Nock, S. H.; Hardy, Alexander T.; Watson, Callum; montague, samantha; Clifford, Hayley; Huissoon, Aarnoud P.; Malcor, Jean-Daniel; Thomas, Mark R.; Pollitt, Alice Y.; Tomlinson, Michael G.; Pratt, Guy; Watson, Steve P.


Ibrutinib and acalabrutinib are irreversible inhibitors of Bruton's tyrosine kinase (Btk) used in the treatment of B cell malignancies. They bind irreversibly to cysteine 481 of Btk, blocking autophosphorylation on tyrosine (Y) 223 and phosphorylation of downstream substrates including phospholipase-ɣ2 (PLCɣ2). In the present study, we demonstrate that concentrations of ibrutinib and acalabrutinib that block Btk kinase activity as shown by loss of phosphorylation at Y223 and PLCɣ2 delay but do...[Show more]

CollectionsANU Research Publications
Date published: 2018
Type: Journal article
Source: Haematologica
DOI: 10.3324/haematol.2018.193391
Access Rights: Open Access


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